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X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein

Squaramides constitute a novel class of RNA polymerase inhibitors of which genetic evidence and computational modeling previously have suggested an inhibitory mechanism mediated by binding to the RNA polymerase switch region. An iterative chemistry program increased the fraction unbound to human pla...

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Bibliografiske detaljer
Udgivet i:J Med Chem
Main Authors: Molodtsov, Vadim, Fleming, Paul R., Eyermann, Charles J., Ferguson, Andrew D., Foulk, Melinda A., McKinney, David C., Masse, Craig E., Buurman, Ed T., Murakami, Katsuhiko S.
Format: Artigo
Sprog:Inglês
Udgivet: 2015
Fag:
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4658208/
https://ncbi.nlm.nih.gov/pubmed/25798859
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.5b00050
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